ziconotide indications/contra

Stem definitionDrug idCAS RN
peptides and glycopeptides 2878 107452-89-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • ziconotide
  • prialt
  • omega-Conopeptide MVIIA (Conus)
  • ziconotide acetate
Ziconotide binds to N-type calcium channels located on the primary nociceptive (A-delta and C) afferent nerves in the superficial layers (Rexed laminae I and II) of the dorsal horn in the spinal cord. Although the mechanism of action of ziconotide has not been established in humans, results in animals suggest that its binding blocks N-type calcium channels, which leads to a blockade of excitatory neurotransmitter release from the primary afferent nerve terminals and antinociception.
  • Molecular weight: 2639.14
  • Formula: C102H172N36O32S7
  • CLOGP: 0
  • LIPINSKI: 3
  • HAC: 68
  • HDO: 42
  • TPSA: 1133.84
  • ALOGS: -3.05
  • ROTB: 38

Drug dosage:

DoseUnitRoute
12 mcg P

Approvals:

DateAgencyCompanyOrphan
Dec. 28, 2004 FDA JAZZ PHARMS INTL

FDA Adverse Event Reporting System

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MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Device issue 327.46 38.08 67 631 6309 3378852
Confusional state 308.16 38.08 90 608 37908 3347253
Pain 295.16 38.08 101 597 71456 3313705
Hallucination, auditory 220.42 38.08 44 654 3597 3381564
Hallucination 173.09 38.08 46 652 13294 3371867
Psychotic disorder 141.58 38.08 36 662 8698 3376463
Mental status changes 141.03 38.08 37 661 10110 3375051
Nausea 111.87 38.08 61 637 129584 3255577
Drug withdrawal syndrome 99.08 38.08 29 669 11756 3373405
Urinary retention 92.61 38.08 25 673 7547 3377614
Dizziness 85.55 38.08 43 655 76469 3308692
Hallucination, visual 80.02 38.08 20 678 4456 3380705
Burning sensation 79.58 38.08 23 675 8881 3376280
Somnolence 73.97 38.08 30 668 32174 3352987
Dysgeusia 73.93 38.08 23 675 11401 3373760
Headache 72.57 38.08 41 657 91939 3293222
Memory impairment 71.83 38.08 24 674 14914 3370247
Gait disturbance 70.93 38.08 28 670 27964 3357197
Vomiting 70.86 38.08 40 658 89491 3295670
Drug ineffective 68.77 38.08 43 655 116047 3269114
Aphasia 67.00 38.08 19 679 6842 3378319
Muscle spasms 64.96 38.08 26 672 26877 3358284
Insomnia 64.20 38.08 28 670 35870 3349291
Depression 61.44 38.08 28 670 39742 3345419
Suicidal ideation 60.28 38.08 22 676 17683 3367478
Agitation 57.99 38.08 22 676 19684 3365477
Fall 56.65 38.08 30 668 58853 3326308
Hypoaesthesia 56.37 38.08 23 675 24916 3360245
Back pain 56.30 38.08 26 672 37979 3347182
Anxiety 55.26 38.08 26 672 39603 3345558

Pharmacologic Action:

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SourceCodeDescription
ATC N02BG08 NERVOUS SYSTEM
ANALGESICS
OTHER ANALGESICS AND ANTIPYRETICS
Other analgesics and antipyretics
FDA MoA N0000020069 N-Calcium Channel Receptor Antagonists
FDA EPC N0000175697 N-type Calcium Channel Antagonist
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D002317 Cardiovascular Agents
MeSH PA D002491 Central Nervous System Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D018696 Neuroprotective Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D020011 Protective Agents
MeSH PA D018689 Sensory System Agents

Drug Use (View source of the data)

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DiseaseRelationSNOMED_IDDOID
Pain in spine indication 48926009
Severe pain indication 76948002
Chronic pain indication 82423001
Chronic Pain with Opioid Tolerance indication
Blood coagulation disorder contraindication 64779008 DOID:1247
Psychotic disorder contraindication 69322001
Increased Creatine Phosphokinase contraindication

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

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Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
100MCG/1ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 ANALGESIA
100MCG/1ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 TREATMENT OF PAIN
100MCG/1ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 ANALGESIA
100MCG/1ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 TREATMENT OF PAIN
100MCG/1ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 9707270 Oct. 1, 2024 TREATMENT OF SEVERE CHRONIC PAIN VIA INTRATHECAL INFUSION OF ZICONOTIDE IN PATIENTS ALSO RECEIVING MORPHINE
200MCG/2ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 ANALGESIA
200MCG/2ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 TREATMENT OF PAIN
200MCG/2ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 ANALGESIA
200MCG/2ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 TREATMENT OF PAIN
200MCG/2ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 DISCN INJECTABLE INTRATHECAL 9707270 Oct. 1, 2024 TREATMENT OF SEVERE CHRONIC PAIN VIA INTRATHECAL INFUSION OF ZICONOTIDE IN PATIENTS ALSO RECEIVING MORPHINE
500MCG/20ML (25MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 ANALGESIA
500MCG/20ML (25MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 TREATMENT OF PAIN
500MCG/20ML (25MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 ANALGESIA
500MCG/20ML (25MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 TREATMENT OF PAIN
500MCG/20ML (25MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 9707270 Oct. 1, 2024 TREATMENT OF SEVERE CHRONIC PAIN VIA INTRATHECAL INFUSION OF ZICONOTIDE IN PATIENTS ALSO RECEIVING MORPHINE
500MCG/5ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 ANALGESIA
500MCG/5ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8653033 Oct. 1, 2024 TREATMENT OF PAIN
500MCG/5ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 ANALGESIA
500MCG/5ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 8765680 Oct. 1, 2024 TREATMENT OF PAIN
500MCG/5ML (100MCG/ML) PRIALT JAZZ PHARMS INTL N021060 Dec. 28, 2004 RX INJECTABLE INTRATHECAL 9707270 Oct. 1, 2024 TREATMENT OF SEVERE CHRONIC PAIN VIA INTRATHECAL INFUSION OF ZICONOTIDE IN PATIENTS ALSO RECEIVING MORPHINE

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent N-type calcium channel subunit alpha-1B Ion channel BLOCKER UNKNOWN CHEMBL
Voltage-dependent N-type calcium channel subunit alpha-1B Unclassified BLOCKER IC50 10.30 IUPHAR
Voltage-dependent P/Q-type calcium channel subunit alpha-1A Unclassified BLOCKER IC50 6.30 IUPHAR

External reference:

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IDSource
4024901 VUID
N0000171594 NUI
C0211011 UMLSCUI
2536 IUPHAR_LIGAND_ID
D06363 KEGG_DRUG
7I64C51O16 UNII
7694 INN_ID
68503 RXNORM
416512006 SNOMEDCT_US
416293004 SNOMEDCT_US
d05424 MMSL
4024901 VANDF
N0000023083 NDFRT
N0000171594 NDFRT
008810 NDDF
DB06283 DRUGBANK_ID
CHEMBL1795072 ChEMBL_ID
CHEMBL2103752 ChEMBL_ID
16135415 PUBCHEM_CID
914454-03-8 SECONDARY_CAS_RN
C078452 MESH_SUPPLEMENTAL_RECORD_UI
CHEBI:135912 CHEBI

Pharmaceutical products:

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ProductCategoryIngredientsNDCFormQuantityRoute MarketingLabel
Prialt HUMAN PRESCRIPTION DRUG LABEL 1 18860-720 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 17 sections
Prialt HUMAN PRESCRIPTION DRUG LABEL 1 18860-722 INJECTION, SOLUTION 100 ug INTRATHECAL NDA 17 sections
Prialt HUMAN PRESCRIPTION DRUG LABEL 1 18860-723 INJECTION, SOLUTION 25 ug INTRATHECAL NDA 17 sections